Antitumor agent-55

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Antitumor agent-55 

Antitumor agent-55 (compound 5q) 是一种有效的抗肿瘤剂。Antitumor agent-55 有效抑制PC3，其 IC50 为 0.91 μM。Antitumor agent-55 能有效抑制 PC3 的菌落形成，抑制细胞迁移。Antitumor agent-55 诱导PC3 G1/S期阻滞和凋亡 (apoptosis)。

Antitumor agent-55

Antitumor agent-55 Chemical Structure

CAS No. : 2522594-49-4

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生物活性

Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3[1].

体外研究
(In Vitro)

Antitumor agent-55 (compound 5q) shows inhibitory activity against MCF-7, PC3, MGC-803, PC9, and WPMY-1 (normal human prostatic stromal myofibroblast cell line), with IC50 values of 11.54 ± 0.18, 0.91 ± 0.31, 8.21 ± 0.50, 34.68 ± 0.67, and 48.15 ± 0.33, respectively[1].
Antitumor agent-55 (0-10 μM, 24-72 h) significantly inhibits the proliferation of PC3 cells dose- and time-dependently[1].
Antitumor agent-55 (0-4 μM, 24 h) increases the G1/S phase population, and dose-dependently elevates the expression of p27 protein[1].
Antitumor agent-55 (0-4 μM, 24-48 h) dose-dependently induces the accumulation of ROS, and induces apoptosis of PC3 cells through activating the two apoptotic signaling pathways simultaneously[1].
Antitumor agent-55 (0-1 μM, 48 h) effectively inhibits the wound healing and the migration of PC3 cells in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: PC3 cells[1]
Concentration: 0, 0.156, 0.313, 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24, 48, 72 h
Result: Significantly inhibited the proliferation of PC3 cells dose- and time-dependently, formed fewer and smaller colonies.

Cell Cycle Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly increased the G1/S phase population while decreased G2/M content at high concentration in PC3 cells.

Western Blot Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 24 h， 48 h
Result: Dose-dependently elevated the expression of p27 protein, markedly elevated the expression of pro-apoptotic Bax and P53 while anti-apoptotic Bcl-2 expression was down-regulated, and significantly increased the expression of cleaved caspase 3/9 and cleaved PARP in a dose-dependent manner.

Apoptosis Analysis

Cell Line: PC3 cells[1]
Concentration: 0, 1, 2, 4 μM
Incubation Time: 48 h
Result: Dose-dependently led to significant increase of apoptotic population, and the apoptotic percentage was up to 70.7% at 4 μM, which was far higher than the control group (3.5%).

分子量

598.72

Formula

C32H34N6O4S
CAS 号

2522594-49-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lu N, Huo JL, Wang S, Yuan XH, Liu HM. Drug repurposing: Discovery of troxipide analogs as potent antitumor agents. Eur J Med Chem. 2020;202:112471.

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